Signaling Pathway

Deubiquitinase

Deubiquitinase

Related Products

PDF File 0.28MB

Deubiquitinases (DUBs) are a large group of proteases that cleave ubiquitin from proteins and other molecules. Ubiquitin is attached to proteins in order to regulate the degradation of proteins via the proteasome and lysosome; coordinate thecellular localisation of proteins; activate and inactivate proteins; and modulate protein-protein interactions. DUBs can reverse these effects by cleaving the peptide or isopeptide bond between ubiquitin and its substrate protein. In humans there are nearly 100 DUB genes, which can be classified into two main classes: cysteine proteases and metalloproteases. The cysteine proteases comprise ubiquitin-specific proteases (USPs), ubiquitin C-terminal hydrolases (UCHs), Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU). The metalloprotease group contains only the Jab1/Mov34/Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases. DUBs play several roles in the ubiquitin pathway. One of the best characterised functions of DUBs is the removal of monoubiqutin and polyubiquitin chainsfrom proteins.

Deubiquitinase Inhibitors & Modulators (17)

Product Name Catalog No. Brief Description
b-AP15

HY-13989

b-AP15(NSC687852) is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14 of the 26S proteasome.

DUBs-IN-1

HY-50736

DUBs-IN-1 is a potent deubiquitinase enzyme inhibitor with IC50s of 18 uM/0.71 uM for USP7/USP8 respectively.

DUBs-IN-2

HY-50737A

DUBs-IN-2 is a potent deubiquitinase enzyme inhibitor with IC50s of 7.2 uM/0.93 uM for USP7/USP8 respectively.

DUBs-IN-3

HY-50737

DUBs-IN-3 is a potent deubiquitinase enzyme inhibitor with IC50s of 3.1 uM for USP8; >30 fold selectivity over USP7 (IC50 > 100 uM).

HBX 19818

HY-17540

HBX 19818 is a selective USP7 inhibitor with IC50 of 28.1 uM .

LDN-57444

HY-18637

LDN-57444 is a potent, reversible, competitive and active site-directed inhibitor of UCHL1 with Ki of 0.4 uM.

ML-323

HY-17543

ML323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay and 174 nM and 820 nM in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) and monoubiquitinated PCNA (Ub-PCNA) as substrates, respectively.

NSC632839

HY-100708

NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.

P 22077

HY-13865

P22077 is a potent inhibitor of ubiquitin-specific protease (USP) 7 (EC50=8.6 uM), P22077 also inhibits the closely related deubiquitinase (DUB) USP47.

P005091

HY-15667

P005091(P5091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM.

PR-619

HY-13814

PR-619 is a broad-range DUB inhibitor with potential for further development as a chemotherapeutic agent in cancer therapy.

SJB2-043

HY-15757

SJB2-043 is one of analogs/derivatives of C527, which is a novel and potent USP1 (ubiquitin-specific protease 1) inhibitor.

SJB3-019A

HY-80012

SJB3-019A is a potent and novel usp1 inhibitor.

USP7-IN-1

HY-16709

USP7-IN-1 is a novel selective and reversible inhibitor of USP7 with IC50 of 33 uM; less or no inhibition on USP5, USP8, Uch-L1, Uch-L3 and Caspase(IC50>200 uM); HCT116 cell viability GI50 is 67 uM.

USP7-USP47 inhibitor

HY-13487

USP7/USP47 inhibitor is a potent and dual inhibitor of USP7/USP47 with IC50s of 0.42 uM(USP7) and 1.0 uM(USP47).

VLX1570

HY-12471

VLX1570 is a competitive inhibitor of proteasome DUB activity with IC50 ranging from 4.2 uM to 8.6 uM.

WP1130

HY-13264

WP1130(Degrasyn) is a novel selective small molecular deubiquitinase (USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and a Bcr/Abl destruction pathway activator with an IC50 of 1.8 μM for K562 cells.